Organic compounds -- part of the class 532-570 series – Organic compounds – Phosphorus esters
Patent
1989-03-14
1992-02-25
Shah, Mukund J.
Organic compounds -- part of the class 532-570 series
Organic compounds
Phosphorus esters
536 64, 536 29, 558199, 558200, 562 10, C07F 130, C07F 936, C07H 15252, C07H 1702
Patent
active
050915525
ABSTRACT:
A compound having the structure: ##STR1## wherein R is CH.sub.3, C.sub.2 H.sub.5, C.sub.3 H.sub.7, t--C.sub.4 H.sub.9 or C.sub.6 H.sub.5 ; R.sup.1 is NH.sub.2, NHCH.sub.3, NHC.sub.2 H.sub.5, NHC.sub.3 H.sub.7, NHC.sub.4 H.sub.9, NHCH.sub.2 CH.sub.2 Cl, NHC.sub.6 H.sub.5, N(CH.sub.3).sub.2, N(C.sub.2 H.sub.5).sub.2, N(C.sub.3 H.sub.7).sub.2, NCH.sub.3 (C.sub.2 H.sub.5), NCH.sub.3 (C.sub.3 H.sub.7), N(CH.sub.2 CH.sub.2 Cl).sub.2, NHOH, NHNHCO.sub.2 CH.sub.2 C.sub.6 H.sub.5, NHNHCO.sub.2 C(CH.sub.3).sub.3, OCH.sub.3, OC.sub.2 H.sub.5, OC.sub.3 H.sub.7, OC.sub.4 H.sub.9, OC.sub.6 H.sub.5, OC.sub.2 C.sub.6 H.sub.5, CH.sub.3, C.sub.2 H.sub.5, C.sub.3 H.sub.7, C.sub.4 H.sub.9, CH.sub.2 NO.sub.2 or CH.sub.2 NH.sub.2 ; and R.sup.2 is NHCH.sub.2 CH.sub.2 Cl or N(CH.sub.2 CH.sub.2 Cl).sub.2.
These compounds may be used to eliminate occult leukemic clonogenic cells from bone marrow by contacting the bone marrow with a solution comprising levels of said compound sufficient to eliminate occult leukemic clonogenic cells. Analogously, tumor cells in a host or organ of a host may be eliminated by treatment of the host or host's organ with a compound of this description.
Compounds of this description are stable aldophosphamide analogs activatable by the action of an esterase and a subsequent E-2 elimination reaction to form acrolein and a phosphoramidic mustard of the formula:
A stable aldophosphamide analog activatable by the action of an esterase and a subsequent spontaneous E-2 elimination reaction to form acrolein and a phosphoramidic mustard, said phosphoramidic mustard having the formula ##STR2## R is NH.sub.2, NHCH.sub.3, NHC.sub.2 H.sub.5, NHC.sub.3 H.sub.7, NHC.sub.4 H.sub.9, NHCH.sub.2 CH.sub.2 Cl, NHC.sub.6 H.sub.5, N(CH.sub.3).sub.2, N(C.sub.2 H.sub.5).sub.2, N(C.sub.3 H.sub.7 (.sub.2, NCH.sub.3 (C.sub.2 H.sub.5), NCH.sub.3 (C.sub.3 H.sub.7), N(CH.sub.2 CH.sub.2 Cl).sub.2, NHOH, NHNHCO.sub.2 CH.sub.2 C.sub.6 H.sub.5, NHNHCO.sub.2 C(CH.sub.3).sub.3, OCH.sub.3, OC.sub.2 H.sub.5, OC.sub.3 H.sub.7, OC.sub.4 H.sub.9, OC.sub.6 H.sub.5, OC.sub.2 C.sub.6 H.sub.5, CH.sub.3, C.sub.2 H.sub.5, C.sub.3 H.sub.7, C.sub.4 H.sub.9, CH.sub.2 NO.sub.2 or CH.sub.2 NH.sub.2 ; and R.sup.1 is NHCH.sub.2 CH.sub.2 Cl or N(CH.sub.2 CH.sub.2 Cl).sub.2.
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Bernhardt E.
Board of Regents , The University of Texas System
Shah Mukund J.
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